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Literature summary for 2.4.2.1 extracted from

  • Glavas-Obrovac, L.; Suver, M.; Hikishima, S.; Hashimoto, M.; Yokomatsu, T.; Magnowska, L.; Bzowska, A.
    Antiproliferative activity of purine nucleoside phosphorylase multisubstrate analogue inhibitors containing difluoromethylene phosphonic acid against leukaemia and lymphoma cells (2010), Chem. Biol. Drug Des., 75, 392-399.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(+/-)-cis-1,1-difluoro-2-(tetrahydro-3-piranyl)ethylphosphonic acid with (hypoxanthine-9-yl)methyl aglycone multisubstrate analogue inhibitor Bos taurus
(+/-)-cis-1,1-difluoro-2-(tetrahydro-3-piranyl)ethylphosphonic acid with (hypoxanthine-9-yl)methyl aglycone multisubstrate analogue inhibitor Homo sapiens
9-(2'-benzyl-5',5'-difluoro-5'-phosphonopentyl)guanine multisubstrate analogue inhibitor Bos taurus
9-(2'-benzyl-5',5'-difluoro-5'-phosphonopentyl)guanine multisubstrate analogue inhibitor Homo sapiens
9-(5',5'-difluoro-5'-phosphonobutyl)-9-deazaguanine multisubstrate analogue inhibitor Bos taurus
9-(5',5'-difluoro-5'-phosphonobutyl)-9-deazaguanine multisubstrate analogue inhibitor Homo sapiens
9-(5',5'-difluoro-5'-phosphonoheptyl)-9-deazaguanine multisubstrate analogue inhibitor Bos taurus
9-(5',5'-difluoro-5'-phosphonoheptyl)-9-deazaguanine multisubstrate analogue inhibitor Homo sapiens
9-deazaguanine multisubstrate analogue inhibitor Bos taurus
9-deazaguanine multisubstrate analogue inhibitor Homo sapiens
additional information multisubstrate analogue inhibitors with 9-deazaguanine aglycone have better anti-leukaemic and anti-lymphoma activities compared to the guanine and hypoxanthine analogues, and applied in the concentration of 100 microM, cause a statistically significant decrease in the cell viability in all human leukemia and lymphoma cells used. No differences are observed between the effects on the growth of tumour cells sensible to the inhibition of purine nucleoside phosphorylase, such as human adult T-cell leukemia and lymphoma cells, and other investigated cells Homo sapiens

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
CCRF-CEM cell
-
Homo sapiens
-
erythrocyte
-
Homo sapiens
-
HL-60 cell
-
Homo sapiens
-
HUT-78 cell
-
Homo sapiens
-
JURKAT cell
-
Homo sapiens
-
K-562 cell
-
Homo sapiens
-
lymphocyte
-
Homo sapiens
-
MOLT cell
-
Homo sapiens
-
RAJI cell
-
Homo sapiens
-
spleen of calf Bos taurus
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000044
-
9-(5',5'-difluoro-5'-phosphonobutyl)-9-deazaguanine pH 7.0, 25°C Bos taurus
0.0000053
-
9-(5',5'-difluoro-5'-phosphonoheptyl)-9-deazaguanine erythrocyte enzyme, pH 7.0, 25°C Homo sapiens
0.0000056
-
9-deazaguanine erythrocyte enzyme, pH 7.0, 25°C Homo sapiens
0.0000057
-
9-(5',5'-difluoro-5'-phosphonoheptyl)-9-deazaguanine pH 7.0, 25°C Bos taurus
0.0000061
-
9-deazaguanine pH 7.0, 25°C Bos taurus
0.0000072
-
(+/-)-cis-1,1-difluoro-2-(tetrahydro-3-piranyl)ethylphosphonic acid with (hypoxanthine-9-yl)methyl aglycone erythrocyte enzyme, pH 7.0, 25°C Homo sapiens
0.0000075
-
9-(2'-benzyl-5',5'-difluoro-5'-phosphonopentyl)guanine pH 7.0, 25°C Bos taurus
0.0000076
-
9-(2'-benzyl-5',5'-difluoro-5'-phosphonopentyl)guanine erythrocyte enzyme, pH 7.0, 25°C Homo sapiens
0.0000081
-
9-(5',5'-difluoro-5'-phosphonobutyl)-9-deazaguanine erythrocyte enzyme, pH 7.0, 25°C Homo sapiens
0.0000112
-
(+/-)-cis-1,1-difluoro-2-(tetrahydro-3-piranyl)ethylphosphonic acid with (hypoxanthine-9-yl)methyl aglycone pH 7.0, 25°C Bos taurus